Serotonin 3 Receptor Antagonist Market: Competitive Landscape, Pipeline, and Market Analysis 2022

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Serotonin type 3 (5-HT3) receptors are pentameric ion channels belonging to the superfamily of Cys-loop receptors. Depending on their neural localization, 5-HT(3) receptors are known to be expressed in regions involved in the vomiting reflex, processing of pain, the reward system, cognition, and anxiety control, and in the periphery, they are known to be involved in emesis, pain disorders, drug addiction, psychiatric and GI disorders. Serotonin receptor (5-HT3) antagonists block serotonin both peripherally, on gastrointestinal vagal nerve terminals, and centrally in the chemoreceptor trigger zone, resulting in powerful antiemetic effects. Both orally and intravenously administered 5-HT3 blockers are indicated for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy including high-dose cisplatin therapy, and radiotherapy. Pfizer, Novartis, Sanofi, Roche, ADial Pharmaceuticals, and Das Therapeutics are currently providing serotonin 3 receptor antagonists for the treatment of cancer patients in the market.

Key Developments

  • In Jan 2023, Samyang Group’s Emestop (Ramosetron Hydrochloride)’s comparison with Palonosetron in preventing postoperative nausea and vomiting in a meta-analysis resulted in no significant differences between the two drugs.
  • In April 2023, Eisai and Merck’s E7386 in a phase 1b study in combination with Lenvatinib in patients with advanced hepatocellular carcinoma showed some promising activity.

Approved Drug Molecules for Serotonin 3 Receptor Antagonist

  • SUSTOL (Granisetron)
  • ADDYI (Flibanserin)
  • Akynzeo (Netupitant and palonosetron)
  • Auvelity (Dextromethorphan HBr -bupropion HCL)
  • Emend (Aprepitant)
  • Zofran (Ondansetron HCL)
  • Invega (Paliperidone)
  • Pepaxto (Melphalan flufenamide)
  • Vraylar (cariprazine)
  • Lybalvi (Olanzapine and Samidorphan)

Pipeline Molecules - Serotonin 3 receptor Antagonists

  • Trenzapride (Azm 112) - Atlantic Healthcare
  • Cvn-058 - Cerevance
  • Granisetron Intranasal (Trg) - Shin Nippon Biomedical Labs
  • Granisetron Transdermal (Syb-0701) - Synmosa Biopharma, SymBio Pharma
  • Ondansetron Ultra-Low Dose (Ad04) - ADial Pharmaceuticals
  • Ondansetron pyridostigmine (DAS-001) - DAS Therap
  • Tedatioxetine (Lu Aa24530) - Takeda, Lundbeck
  • R-azasetron besylate (SENS-401) - Sensorion
  • TAK-058 - Takeda

Clinical Activity and Development of Serotonin 3 Receptor Antagonists

In the Serotonin 3 receptor antagonists, currently, there are 29 products, being operated by 32 pharmaceutical companies, including both approved drugs and drugs in clinical trials.

  • In Jan 2021, Synmosa Biopharma, SymBio, and Abeillie Pharma’s Granisetron transdermal (SyB-0701) were compared with oral Granisetron in a meta-analysis, resulting in better achievement of oral Granisetron for completely controlling CINV in patients receiving chemotherapy.
  • In Jan 2023, Samyang Groups’s Emestop’s (Ramosetron HCL) efficacy was compared with aqueous cinnamon extract, for partially attenuated bowel symptoms in the IBS model, which acted by directly inhibiting Tph1 expression and controlling 5-HT synthesis.
  • In Mar 2023, Takeda and Lundbeck’s Trintellix (Vortioxetine) and tedatioxetin (Lu AA24530), and Lundbeck and Otsuka’s Rexulti (Brexipiprazole), in a study it was observed that Asian carriers of CYP2D6 decreased function alleles tended to exhibit higher CYP2D6 activity compared to Caucasians and Africans Americans, inter-ethnic differences within the CYP2D6 phenotype and genotype groups appeared to be driven by differences in CYP2D6 allele frequencies across ethnicities rather than inter-ethnic differences in enzyme activity for individuals carrying identical CYP2D6 genotypes.

Target Indication Analysis of Serotonin 3 Receptor Antagonists

Serotonin type 3 (5-HT3) antagonists are primarily used for the prevention of nausea and vomiting induced due to chemotherapy. Other indications of 5-HT3 antagonists include major depressive disorder, postoperative nausea and vomiting, diarrhea-predominant IBS, insomnia, and as an appetizer. Moreover, there are several clinical trials are presently being conducted for the treatment of bipolar depression, schizophrenia, cognitive impairment with primary psychotic disorder, breast carcinoma, gallbladder cancer, malignant neoplasm, and Alzheimer’s disease by using 5-HT3 antagonists.

Frequently Asked Questions

Sustol (Granisetron), Addyi (Flibanserin), Emend (Aprepitant), and Zafron (Ondansetron) are the approved molecule in the Serotonin 3 receptor antagonist.

The global sale of Sustol for 2022 was US$ 10.2 million.

Pfizer, Novartis, Sanofi, Roche, ADial Pharmaceuticals, and Das Therapeutics are a few major players in the Serotonin 3 receptor antagonist space.

Bipolar depression, schizophrenia, cognitive impairment with primary psychotic disorder, breast carcinoma, gallbladder cancer, malignant neoplasm, and alzheimer’s disease are some of the indications on which companies could focus for the expansion of the serotonin 3 receptor antagonists market.

Key Features of the Reports

  • The report provides granular level information about the market size, regional market share, historic market (2019-2023), and forecast (2024-2030)
  • The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
  • The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
  • The report tracks recent innovations, key developments, and start-up details that are actively working in the market
  • The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
  • Pfizer (USA)
  • Roche (Switzerland)
  • Heron Therapeutics (USA)
  • Atlantic Healthcare (UK)
  • ADial Pharmaceuticals (USA)
  • DAS Therapeutics (USA)
  • Helsinn Therapeutics (USA)
  • Eisai Co. Ltd. (Japan)
  • Novartis (Switzerland)
  • Takeda Pharmaceuticals (USA)

Adjacent Markets